Patents Assigned to Merck Sharp
  • Pharmaceutical composition of a tachykinin receptor antagonist
    Patent number: 8258132
    Abstract: The present invention is directed to novel pharmaceutical compositions of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine. The pharmaceutical compositions of this invention useful in the treatment or prevention of disorders such as psychiatric disorders including depression and anxiety, inflammatory diseases and emesis.
    Type: Grant
    Filed: December 9, 2002
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: H. William Bosch, Elaine Liversidge, Suhas D. Shelukar, Karen C. Thompson
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8258135
    Abstract: The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald K. Chang, Scott D. Kuduk
  • Crystalline salt form of an antidiabetic compound
    Patent number: 8258161
    Abstract: A novel crystalline anhydrous toluenesulfonic acid salt form of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety is stable and non-hygroscopic. The crystalline salt form is useful for making pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Aquiles E. Leyes
  • Piperidine derivatives
    Patent number: 8252803
    Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: August 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Alexey A. Rivkin
  • Angiotensin II receptor antagonists
    Patent number: 8252825
    Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is 1) —(CH2)3R5, 2) —C(O)(CH2)2R5, 3) —C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) —C(R1R2)OC(O)CH2CH2R5, 5) —C(R1R2)OC(O)OCH2CH2C(R3R4)R5, provided that when Y is —C(O)(CH2)2R5, then R is R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is —CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: August 28, 2012
    Assignees: NicOx, Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Nicoletta Almirante, Silvia Stefanini, Laura Storoni, Stefano Biondi, Ennio Ongini
  • Hexahydro-1H-4,7-methanoisoindole-1,3-dione compounds
    Patent number: 8252799
    Abstract: The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R1 is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R1 and the hydroxyl group on the ring are attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: August 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
  • HEXAHYDROCYCLOPENTYL[F]INDAZOLE PYRIDYL ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS
    Publication number: 20120214846
    Abstract: The present invention encompasses compounds of Formula (I): or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 26, 2010
    Publication date: August 23, 2012
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Helen J. Mitchell, William P. Dankulich, Mildred K. Kaufman, Robert S. Meissner
  • 2-[1-PHENYL-5-HYDROXY-4a-SUBSTITUTED-HEXAHYDROCYCLOPENTA[F]INDAZOL-5-YL]ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS
    Publication number: 20120214847
    Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 26, 2010
    Publication date: August 23, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, James J. Perkins, Jesse J. Manikowski, Pablo de Leon, Robert S. Meissner
  • Hydroxymethyl pyrrolidines as ?3 adrenergic receptor agonists
    Patent number: 8247415
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: April 2, 2009
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
  • P2Xreceptor antagonists for treatment of pain
    Patent number: 8247401
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • Pyridyl piperidine orexin receptor antagonists
    Patent number: 8242121
    Abstract: The present invention is. directed to pyridyl piperidine compounds of formula (I) which are antagonists of orexin receptors, and which are useful' in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, John D. Schreier
  • Sulphamides for treatment of cancer
    Patent number: 8242103
    Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Triazole derivatives for treating alzheimer'S disease and related conditions
    Patent number: 8242150
    Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.
    Type: Grant
    Filed: June 9, 2008
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
    Patent number: 8242257
    Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonid Beigelman, James McSwiggen
  • Thiazolyl mGluR5 antagonists and methods for their use
    Patent number: 8242143
    Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
  • COMBINATION THERAPY USING A BETA 3 ADRENERGIC RECEPTOR AGONISTS AND AN ANTIMUSCARINIC AGENT
    Publication number: 20120202819
    Abstract: Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.
    Type: Application
    Filed: September 27, 2010
    Publication date: August 9, 2012
    Applicant: Merck Sharp & Dohme Corporation
    Inventors: Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
    Patent number: 8236944
    Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: August 7, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonid Beigelman, James McSwiggen
  • TERTIARY AMIDE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20120196901
    Abstract: The present invention is directed to tertiary amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 2, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
  • Process for the production of a crystalline glucagon receptor antagonist compound
    Patent number: 8232413
    Abstract: The present invention relates to a process for the production of crystalline particles of a glucagon receptor antagonist compound. The process includes the steps of generating microseeds and subjecting the microseeds to a crystallization process. The resulting crystalline particles have a mean particle size of less than about 100 mm. The present invention also provides for a pharmaceutical composition which includes the crystalline particles produced by the method described herein and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: July 31, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Benjamin M. Cohen, Daniel J. Kumke, Lushi Tan, Aaron S. Cote
  • Pyridazinone derivatives useful as glucan synthase inhibitors
    Patent number: 8232274
    Abstract: Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: July 31, 2012
    Assignees: Albany Molecular Research, Inc., Merck Sharp & Dohme Corp.
    Inventors: Pauline C. Ting, Robert G. Aslanian, Jianhua Cao, David Won-Shik Kim, Rongze Kuang, Gang Zhou, Robert Jason Herr, Andrew John Zych, Jinhai Yang, Heping Wu, Nicolas Zorn